Copper‐Catalyzed N‐Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore

Inexpensive copper catalysts allow for efficient syntheses of N‐aryl‐, N‐acyl‐, or N‐H‐(aza)indoles starting from ortho‐alkynylbromoarenes. The broad scope of this domino N‐arylation/hydroamin(d)ation process is highlighted by the synthesis of highly functionalized indoles, as well as of a Chek1/KDR...

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Veröffentlicht in:Advanced synthesis & catalysis 2009-05, Vol.351 (7‐8), p.1064-1072
Hauptverfasser: Ackermann, Lutz, Barfüßer, Sebastian, Potukuchi, Harish K.
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container_title Advanced synthesis & catalysis
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creator Ackermann, Lutz
Barfüßer, Sebastian
Potukuchi, Harish K.
description Inexpensive copper catalysts allow for efficient syntheses of N‐aryl‐, N‐acyl‐, or N‐H‐(aza)indoles starting from ortho‐alkynylbromoarenes. The broad scope of this domino N‐arylation/hydroamin(d)ation process is highlighted by the synthesis of highly functionalized indoles, as well as of a Chek1/KDR inhibitor pharmacophore.
doi_str_mv 10.1002/adsc.200900004
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subjects amination
arylation
catalysis
copper
hydroamination
indoles
title Copper‐Catalyzed N‐Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore
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